Laboratory and clinical studies on Cefsulodin (SCE-129, CFS) were performed and the following results were obtained.
1. Serum levels
Mean serum level of CFS was 15.2μg/ml at 15 minutes after a single intravenous injection of 500mg.
In intravenous drip infusion, peak serum levels were observed just after the end of the drip infusion in every dose and period of the injection.
The peak sei um levels weie 26.4μg/ml in 750mg, 42.6μg/ml in 1, 000mg with the one-hour-drip infusion and 14.0μg/m; in 250mg, 21.4μg/ml in 500mg and 30.5 μg/ml in 750mg with the two-hour-drip infusion.
CFS was rapidly excreted from the blood after injection and was detected a little amount (0.9, -3.3μg/ml) in serum in 5-6 hours after the end of injection.
CFS gave the biological half-life of ca. 1.4 hours in every dose and dosing period.
2. Urinary excretion
CFS was excreted in urine well and gave a urinary recovery of 60-80% in hours after the end of injections.
3. Clinical application
CFS was given intravenously or by intravenous drip infusion, a daily dose of 750 or 1, 000mg, for 3-23 days to four patients in a remission stage of acute myelocytic leukemia with such infections as septicemia, urinary tract infections, liver abscess and pnuemonia.
Chemotherapeutic results were excellent in 3 patients and poor in one patient with pneumoina due to CFS-resistant strain of
P. aeruginosa.
No adverse effect was seen in every patient.
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